• Archives of Pharmacal Research
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• v.28 no.5
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• pp.626-635
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• 2005

Liposome as a carrier of topotecan (TPT), a promising anticancer drug, has been reported in attempt to improve the stability and antitumor activity of TPT. However, the biodistr ibution pattern of TPT liposome in vivo and PEG-modified liposome containing TPT have not been studied systemically. In this paper, the in vitro stability and in vivo biodistribution behavior of several liposomes containing TPT with different lipid compositions and PEG-modification were studied. Compared with the 'fluid' liposome (S-Lip) composed of soybean phosphatidylcholine (SPC), the 'solid' liposome (H-Lip) composed of hydrogenated soybean phosphatidylcholine HSPC decreased the leaking efficiency of TPT from liposome and enhanced the stability of liposome in fetal bovine serum (FBS) or human blood plasma (HBP). The results of biodistribution studies in S$_{180}$ tumor-bearing mice showed that liposomal encapsulation increased the concentrations of total TPT and the ratio of lactone form in plasma. Compared with free TPT, S-Lip and H-Lip resulted in 5- and 19- fold increase in the area under the curve (AUC$_{0\rightarrow\propto}$), respectively. PEG- modified H-Lip (H-PEG) showed 3.7-fold increase in AUC$_{0\rightarrow\propto}$ compared with H-Lip, but there was no significant increase in t$_{1/2}$ and AUC$_{0\rightarrow\propto}$ for PEG-modified S-Lip (S-PEG) compared with S-Lip. Moreover, the liposomal encapsulation changed the biodistribution behavior, and H-Lip and H-PEG dramatically increased the accumulation of TPT in tumor, and the relative tumor uptake ratios were 3.4 and 4.3 compared with free drug, respectively. There was also a marked increase in the distribution of TPT in lung when the drug was encapsulated into H-Lip and H-PEG. Moreover, H-PEG decreased the accumulation of TPT in bore marrow compared with unmodified H-Lip. All these results indicated that the membrane fluidity of liposome has an important effect on in vitro stability and in vivo biodistribution pattern of liposomes containing TPT, and PEG-modified 'solid' liposome may be an efficient carrier of TPT.

• Journal of Pharmaceutical Investigation
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• v.40 no.2
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• pp.85-90
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• 2010

Docetaxel-loaded liposomes were prepared by emulsion-solvent evaporation method, then coated with chitosan at room temperature and lyophilized. This system was designed in order to improve solubility and stability of docetaxel in the GI tract for oral drug delivery. The solubilizing effect of some frequently used solubilizers and/or liposome was determined. Among the results docetaxel-loaded liposomes prepared with 0.5% TPGS as a solubilizer showed 100-fold higher solubility than docetaxel. In a stability test, mean particle size of different liposome formulations was measured by a particle size analyzer in simulated gastric fluid (SGF) and in simulated intestinal fluid (SIF). The particle size of uncoated liposomes was significantly increased compared with that of chitosan-coated liposomes in SGF, however, there was no significant difference between coated and uncoated liposome in SIF. It is evident that chitosan-coated liposomes were more stable in GI conditions. The release characteristics of docetaxel-loaded liposomes were also investigated in three buffer solutions (pH 1.2, 4.0, 6.8). Docetaxel release did not occur in pH 1.2 for 4 hrs. However, in pH 4.0 and 6.8 conditions, docetaxel was gradually released over 24 hrs as a sustained release. It seems that aggregation and precipitation of particles by electrostatic interaction might protect docetaxel from being released. In Conclusion, the results from this study show that the chitosan-coated liposomes may be useful in enhancing solubility and GI stability of docetaxel.

• Biotechnology and Bioprocess Engineering:BBE
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• v.11 no.6
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• pp.526-529
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• 2006

The aim of this study was to prepare cyclosporin A-loaded liposome (CyA-Lip) as an oral delivery carrier, with their encapsulation into microspheres based on alginate or extracellular polysaccharide (EPS) p-m10356. The main advantage of liposomes in the microspheres (LIMs) is to improve the restricted drug release property from liposomes and their stability in the stomach environment. Alginate microspheres containing CyA-Lip were prepared with a spray nozzle; CyA-Liploaded EPS microspheres were also prepared using a w/o emulsion method. The shape of the LIMs was spherical and uniform, and the particle size of the alginate-LIMs ranged from 5 to $10\;{\mu}m$, and that of the EPS-LIMs was about $100\;{\mu}m$. In a release test, release rate of CyA in simulated intestinal fluid (SIF) from the LIMs was significantly enhanced compared to that in simulated gastric fluid (SGF). In addition, the CyA release rates were slower from formulations containing the liposomes compared to the microspheres without the liposome. Therefore, alginate-and EPS-LIMs have the potential for the controlled release of CyA and as an oral delivery system.

• The Journal of the Convergence on Culture Technology
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• v.8 no.6
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• pp.605-614
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• 2022

In this study, oregano was extracted by supercritical extraction and hydrothermal extraction method. In vitro experiments such as antimicrobial and antioxidant activity test were performed. As a result of the disc diffusion method, only the supercritical extracts formed a clear zone. The MIC for S. aureus was found only in the supercritical fluid extracts and it was 1000 ㎍/mL. The hydrothermal extract's MIC is 125 ㎍/mL for C. acnes. Through biofilm inhibition assay, we found that the supercritical fluid oregano extracts inhibit the biofilm of S. aureus by more than 70% even at low concentrations of 125 ㎍/mL. On the other hand, the antioxidant ability of the hydrothermal extract was better than that of the supercritical fluid extracts. Furthermore, we tried to make a skincare ingredient for atopic dermatitis by utilizing the S. aureus biofilm inhibitory ability of oregano supercritical fluid extracts. Liposome was used to overcome the low solubility of the oregano supercritical fluid extracts and increase stability.

• BMB Reports
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• v.35 no.4
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• pp.358-363
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• 2002

Chemical and photochemical processes during storage and preparation rapidly degrade retinol, the most active form of vitamin A. therefore, the efficacy of incorporation into liposomes in order to modulate the kinetics of retinol degradation was investigated. Retinol was readily incorporated into multilamellar liposomes that were prepared form soybean phosphatidylcholine; the extent of the incorporation was 98.14±0.93% at pH 9.0 at a ratio of 0.01 : 1 (wt:wt) retinol : phospholipid. It was only marginally lower at higher retinol concentrations. The pH of the hydration buffer had a small effect. The incorporation efficiency ranged from 99.25±0.47% at pH 3 to 97.45±1.13% at pH 11. The time course of the retinol degradation in the aqueous solution in liposomes was compared to that of free retinol and free retinol with α-tocopherol under a variety of conditions of pH(3, 7, and 11), temperature(4, 25, 37, and 50℃), and light exposure(dark, visible, and UV). The retinol that was incorporated into the liposomes degraded significantly slower than the free retinol or retinol with α-tocopherol at pH 7 and 11. At pH 3, where the free retinol degrades rapidly, the degradation kinetics were similar in liposomes and the presence of α-tocopherol. At pH 7.0 and 4℃ in the light, for example, free aqueous retinol was completely degraded within 2 days, while only 20% of the retinol in the liposomes were degraded after 8 days. In general, the protective effect of the liposome incorporation was greater at low temperatures, at neutral and high pH, and in the dark. The results suggest that protection is greater in the solid, gel phase than in the fluid liquid crystalline phase lipids. These results indicate that the incorporation into liposomes can extend the shelf-life of retinol under a variety of conditions of temperature, pH, and ambient light conditions.

• Biomedical Science Letters
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• v.17 no.3
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• pp.211-216
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• 2011

The chitosan-coated liposomes (chitosomes) were designed to improve the stability in the gastrointestinal (GI) tract and to enhance the efficacy for oral drug delivery of liposomes. The phosphatic acid (PA)-incorporated anionic liposomes were surface-coated with water soluble chitosan (WSC) by electro-ionic interaction. The shape of the chitosomes observed by transmission electron microscopy (TEM) was spherical in all the formulations and the coating layer by WSC could be founded through TEM images. The mean size and the zeta potential values of the chitosomes increased significantly with depending on the content of WSC added for coating the liposomes. The stability of the chitosomes in the GI tract was confirmed through the change of relative turbidity of the liposomal suspension. The plain liposomes (plasomes) suspension without adding WSC clearly showed the change of relatively turbidity in simulated gastric fluid (SGF), while the change degree of turbidity of the chitosomes in the SGF decreased as increasing of WSC content added for coating liposome. In the 5-CF release study from the plasomes and chitosomes, the plasomes released >90% of the initial 5-CF content at 4 h of release measurement. In contrast, the chitosomes released below 40% of initial content of 5-CF. In conclusion, these results indicate that the chitosomes can be used as a potential carrier for effective oral drug delivery.